Abstract
The objective of the study was the development and in vitro characterization of a self-emulsifying drug delivery system (SEDDS) for the nasal application of dimenhydrinate. Final composition of SEDDS was established based on drug solubility and stability studies. Dimenhydrinate was loaded into the SEDDS pre-concentrates to 7.5% (m/v). The droplet size of the final SEDDS formulations was in a range between 60 and 220 nm. Permeability, as well as tissue toxicity, of the formulations was investigated using bovine nasal mucosa. Enhancement in permeation up to 2.8-fold compared to pure dimenhydrinate was confirmed. Furthermore, toxicity studies did not reveal any serious tissue damages related to the SEDDS. Additionally, irritation potential of SEDDS was evaluated in ciliary beat frequency measurements. Incorporation of dimenhydrinate into SEDDS might therefore be considered as a promising approach within the field of nasal delivery of antiemetics by utilizing permeation enhancement strategy.
Highlights
In recent years, the nasal route has been increasingly investigated for the systemic delivery of drugs
The solubility of dimenhydrinate was examined within the first step of the development of self-emulsifying drug delivery system (SEDDS) in order to find the final composition of the pre-concentrates
Dimenhydrinate possessed the highest solubility in Transcutol HP (HLB 4) followed by Capmul MCM and Capmul propylene glycol (PG)-8
Summary
The nasal route has been increasingly investigated for the systemic delivery of drugs. Small lipophilic drugs are getting well absorbed by the nasal cavity with pharmacokinetic profiles close to those obtained after intravenous injection achieving bioavailability of nearly 100% [3, 4]. Marketed formulations for the nasal administration are used in the therapy of migraine (sumatriptan (Glaxo Smith Kline) and zolmitriptan (Astra Zeneca)), or for the treatment of pain (butorphanol (Bristol-Myers Squibb)) [3, 5]. For the treatment of nausea and vomiting, where the use of the oral route might be complicated or not feasible, nasal administration offers a suitable alternative as a rapid onset of action is provided combined with convenient dosing [6]
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
